Background: Coxsackievirus infections are associated with cases of aseptic meningitis,
encephalitis, myocarditis, and some chronic disease.
Methods: A series of benzo[d][1,2,3]triazol-1(2)-yl derivatives (here named benzotriazol-1(2)-yl)
(4a-i, 5a-h, 6a-e, g, i, j and 7a-f, h-j) were designed, synthesized and in vitro evaluated for cytotoxicity
and antiviral activity against two important human enteroviruses (HEVs) members of the
Picornaviridae family [Coxsackievirus B 5 (CVB-5) and Poliovirus 1 (Sb-1)].
Results: Compounds 4c (CC50 >100 μM; EC50 = 9 μM), 5g (CC50 >100 μM; EC50 = 8 μM), and 6a
(CC50 >100 μM; EC50 = 10 μM) were found active against CVB-5. With the aim of evaluating the
selectivity of action of this class of compounds, a wide spectrum of RNA (positive- and negativesense),
double-stranded (dsRNA) or DNA viruses were also assayed. For none of them, significant
antiviral activity was determined.
Conclusion: These results point towards a selective activity against CVB-5, an important human
pathogen that causes both acute and chronic diseases in infants, young children, and immunocompromised